BI-0252

Name: BI-0252
Brand: TargetMol
SKU: T14554
Rating: 4.5 (1 reviews)

😃Good

Catalog No. T14554Cas No. 1818291-27-8

BI-0252 is an inhibitor of MDM2-p53 (IC50:4 nM). BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft. And it concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis.

BI-0252

😃Good

Catalog No. T14554Cas No. 1818291-27-8

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,820	8-10 weeks	8-10 weeks
50 mg	$2,380	8-10 weeks	8-10 weeks
100 mg	$3,100	8-10 weeks	8-10 weeks

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Resource Download

Product Introduction

Bioactivity

Description	BI-0252 is an inhibitor of MDM2-p53 (IC50:4 nM). BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft. And it concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis.
Targets&IC50	MDM2-p53:4 nM
In vivo	BI-0252 has high po in vivo exposure and good cellular potency[1]. BI-0252 (orally; 25 mg/kg/day for 13 days and 100 mg/kg for 24 h) leads to time-dependent mRNA induction of TP53 target genes including CDKN1a, MDM2, and BBC3[1]. BI-0252 (iv and po; an iv dose of 5 mg/kg and a po dose of 50 mg/kg) showes low clearance in vivo after iv administration and high clearance after po administration.

Chemical Properties

Molecular Weight	566.45
Formula	C₃₀H₂₆Cl₂FN₃O₃
Cas No.	1818291-27-8
Smiles	C(N1[C@@]2([C@H]([C@]3([C@@]1(C[C@@H](N3)C4=CC=C(C(O)=O)C=C4)[H])[H])C5=C(F)C(Cl)=CC=C5)C=6C(NC2=O)=CC(Cl)=CC6)C7CC7
Relative Density.	1.53 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc